卡纳比和塔克罗利斯之间的药物动力学相互作用的第一阶段试验
Gerald C So1, Jessica Bo Li Lu1, Sachiko Koyama1
1Department of Medicine, Indiana University School of Medicine, Indianapolis, Indiana, USA.
Clinical pharmacology and therapeutics
|November 27, 2024
概括
大麻醇显著增加了常见的免疫抑制剂塔克罗利斯的暴露. 这种药物相互作用需要对使用这两种物质的患者进行仔细监测和潜在的剂量调整.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物新陈代谢 药物新陈代谢
- 临床药理学 临床药理学
背景情况:
- 大麻二醇 (CBD) 广泛使用,每6个美国人中就有1个消费大麻衍生产品.
- CBD是已知的细胞染色体P450 3A (CYP3A) 的基质,但其抑制潜力尚未完全理解.
研究的目的:
- 调查CBD抑制CYP3A介导的塔克罗利斯代谢的假设.
- 在健康参与者中量化CBD对塔克罗利斯药理动学的影响.
主要方法:
- 一个开放的,三期的交叉研究,涉及健康的参与者.
- 在14天的CBD稳定状态定位前和后 (5 mg/kg每天两次) 服用单次口服塔克罗利 (5 mg) 剂量.
- 使用UHPLC-MS/MS测量全血塔克罗利斯度,通过非分区分析分析的药理学参数.
主要成果:
- 同时服用CBD导致塔克罗利斯最大度 (Cmax) 增加4.2倍,度-时间曲线 (AUC0-∞) 下的面积增加3.1倍.
- 没有观察到塔克罗利莫斯半衰期 (t1/2) 的显著变化.
- 这些变化具有统计学意义 (P < 0.0001).
结论:
- 在健康个体中,CBD显著增加了对塔克罗利斯的全身暴露.
- 这些发现表明,在移植患者同时服用CBD和tacrolimus时,可能存在显著的药物相互作用.
- 建议在与CBD同时使用时密切监测治疗药物和降低潜在的塔克罗利斯剂量.
相关概念视频
Chemotherapy-Induced Nausea and Vomiting: Cannabinoids
202
Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
Two synthetic agonists of THC,...
Two synthetic agonists of THC,...
202
Clinical Trials: Overview
2.8K
Clinical development focuses on how the drug will interact with the human body and encompasses four key phases of clinical trials, each serving a specific purpose in assessing the safety and effectiveness of new drugs. These phases overlap and build upon one another. Phase I involves a small group of healthy volunteers (typically 20-80 individuals) or, in cases where significant toxicity is expected, patients with the targeted disease, such as cancer or AIDS. The volunteers are tested for...
2.8K
Drug Concentration Versus Time Correlation
631
The plasma drug concentration-time curve is a crucial tool in pharmacokinetics, representing the drug's concentration in plasma at different time intervals post-administration. This curve illustrates the drug's journey from absorption into the systemic circulation, distribution to body tissues, and eventual elimination through excretion or biotransformation.
Two pivotal parameters are the minimum effective concentration (MEC) and the minimum toxic concentration (MTC). The MEC is the...
Two pivotal parameters are the minimum effective concentration (MEC) and the minimum toxic concentration (MTC). The MEC is the...
631


